CN115607539A - Polyphenol compound medicine and slow release method - Google Patents
Polyphenol compound medicine and slow release method Download PDFInfo
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- CN115607539A CN115607539A CN202211268046.2A CN202211268046A CN115607539A CN 115607539 A CN115607539 A CN 115607539A CN 202211268046 A CN202211268046 A CN 202211268046A CN 115607539 A CN115607539 A CN 115607539A
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- coating
- polyphenol compound
- polyphenol
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5015—Organic compounds, e.g. fats, sugars
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
Abstract
The invention relates to a polyphenol compound medicament and a sustained release method, belonging to the technical field of polyphenol compound medicaments.
Description
Technical Field
The invention relates to a polyphenol compound medicine and a sustained release method, belonging to the technical field of polyphenol compound medicines.
Background
Alzheimer's Disease (AD) is a progressive degenerative disease of the nervous system with occult disease, characterized clinically by generalized dementia such as memory impairment, aphasia, disuse, agnosia, impairment of visual spatial skills, impairment of executive function, and personality and behavioral changes, the etiology of which has not been known so far, with patients before age 65 being called alzheimer's disease, and patients after age 65 being called senile dementia.
The polyphenol compound consists of more than 40 chemical components, has the effects of resisting oxidation, strengthening vessel walls, promoting gastrointestinal digestion, reducing blood fat, increasing body resistance, preventing arteriosclerosis and thrombosis, and also has the effects of promoting urination, reducing blood pressure, inhibiting the growth of bacteria and cancer cells and helping digestion, so the polyphenol compound medicine can also improve the symptoms of Alzheimer disease;
the Alzheimer patients have poor self-control ability, and have resistance to medicaments, which is not beneficial to treatment. Therefore, we improve the above and propose polyphenol compounds as drugs and sustained release methods.
Disclosure of Invention
The technical problem to be solved by the invention is as follows: the self-control ability of the Alzheimer patient is poor, and the Alzheimer patient has resistance to medicaments and is not beneficial to treatment.
In order to realize the aim, the invention provides a polyphenol compound medicament, which comprises the following raw materials in parts by weight:
0.5-1.2 parts of polyphenol compound, 3-6 parts of adhesive, 30-60 parts of filler and 5-10 parts of disintegrating agent;
the coating also comprises a coating, wherein the polyphenol compound, the adhesive, the filler and the disintegrant are coated in the coating, a plurality of pores are formed in the outer surface of the coating, and each pore is filled with powdery sugar particles.
Wherein the polyphenol compound, the adhesive, the filler and the disintegrant are mixed and then coated in the coating.
Wherein, the coating is a high molecular film, and the high molecular film is ethyl cellulose or cellulose acetate.
Wherein the powder sugar particles are one of erythritol, stevioside or aspartame.
Wherein the polyphenol compound is one of flavonoid, stilbene, phenolic acid or lignan.
Wherein the adhesive is one of povidone, hypromellose or sodium carboxymethylcellulose.
Wherein the filler is one of starch, microcrystalline cellulose or inorganic calcium salt.
Wherein the inorganic calcium salt is one of calcium sulfate, calcium hydrophosphate or calcium carbonate.
Wherein the disintegrating agent is one of sodium hydroxymethyl starch, low-substituted hydroxypropyl cellulose or cross-linked sodium hydroxymethyl cellulose.
A method for the sustained release of a polyphenol drug comprising:
A. swallowing the polyphenol with water;
B. after swallowing, the powder sugar particles filled in the pores are dissolved in water, the water enters the coating through the pores, so that the medicine in the coating is dissolved into a saturated solution, and the saturated solution continuously flows out from the pores until the dissolution is finished due to the difference of the osmotic pressure inside and outside the coating.
The polyphenol compound medicament and the sustained release method provided by the invention have the beneficial effects that:
1. according to the invention, the pores are formed on the outer surface of the coating, and the powder sugar particles are filled in the pores, so that the finished product has sweet taste, and the sweet taste has higher attraction to patients, thereby reducing the resistance of the patients to the medicine, and being beneficial to use and treatment;
2. the fine holes are filled with the powdery sugar particles, so that the fine holes can be blocked, the leakage of the medicine from the fine holes is reduced, the powdery sugar particles are erythritol, stevioside or aspartame, the erythritol is easily dissolved in water, and the erythritol does not participate in human glucose metabolism and is not converted into glucose in a human body, so that the blood glucose value is not increased, and the powdery sugar particles are suitable for various crowds;
3. the powder sugar grain of filling in the pore is dissolved in water after swallowing, and water passes through in the pore gets into the coating for the medicine in the coating dissolves for saturated solution, the difference of osmotic pressure inside and outside the coating, saturated solution is continuously flowed out by the pore, and until dissolving totally, the setting can make active ingredient slowly precipitate like this, can increase patient's compliance and reduce the side effect of medicine.
Drawings
In order to more clearly illustrate the embodiments of the present invention or the technical solutions in the prior art, the drawings used in the description of the embodiments or the prior art will be briefly described below, and it is obvious that the drawings in the following description are only some embodiments of the present invention, and for those skilled in the art, other drawings can be obtained according to these drawings without creative efforts.
FIG. 1 is a schematic structural diagram of a coating of a polyphenol compound drug provided by the present invention;
FIG. 2 is a schematic sectional view of a part of a coating of a polyphenol compound drug provided by the present invention;
FIG. 3 is a schematic structural view of pores of the polyphenol compound drug provided by the present invention;
FIG. 4 is a table showing the test results of the polyphenol compound drugs provided by the present invention.
100. Coating; 200. fine pores; 300. and (4) powder sugar particles.
Detailed Description
The following detailed description of the embodiments of the present invention is provided in connection with the drawings and examples. The following examples are intended to illustrate the invention, but are not intended to limit the scope of the invention.
Example 1:
as shown in fig. 1, fig. 2 and fig. 3, the present embodiment provides a polyphenol compound drug, which comprises the following raw materials in parts by weight:
0.5 part of polyphenol compound, 3 parts of adhesive, 30 parts of filler and 5 parts of disintegrating agent;
the novel sugar-free tablet further comprises a coating 100, wherein the polyphenol compound, the adhesive, the filler and the disintegrating agent are wrapped in the coating 100, a plurality of fine holes 200 are formed in the outer surface of the coating 100, the powder sugar particles 300 are filled in each fine hole 200, the fine holes 200 are formed in the outer surface of the coating 100, and the powder sugar particles 300 are filled in the fine holes, so that a finished product has sweet taste, and the sweet taste has high attraction to patients, so that the rejection of the patients to medicines is reduced, and the novel sugar-free tablet is beneficial to use and treatment.
In a preferred embodiment, in addition to the above-described embodiment, the coating 100 is coated with a mixture of the polyphenol compound, the binder, the filler and the disintegrant, and the coating 100 protects the polyphenol compound, the binder, the filler and the disintegrant.
In a preferred embodiment, in addition to the above embodiment, the coating 100 is a polymer film, the polymer film is ethyl cellulose, and the polymer film is insoluble in water, and after administration, the coating enters the intestinal tract under the gastrointestinal motility and is finally discharged to the outside of the body.
In a preferred embodiment, in addition to the above embodiment, the powdery sugar particles 300 are erythritol, erythritol particles are easily soluble in water, and erythritol does not participate in human glucose metabolism and is not converted into glucose in the human body, and therefore, the powdery sugar particles are suitable for various people without increasing the blood glucose level.
In a preferred embodiment, in addition to the above-mentioned embodiment, the polyphenol compound is a flavonoid, and the polyphenol compounds used in the present invention are all known in the art, and therefore, the details thereof are not repeated.
In a preferred embodiment, in addition to the above, the binder is povidone, and the binder is used to bond a plurality of substances together.
In a preferred embodiment, in addition to the above embodiment, the filler is starch, and the filler can increase the bulk increase in weight.
In a preferred embodiment, in addition to the above embodiment, the inorganic calcium salt is calcium sulfate.
In addition to the above-mentioned embodiments, a disintegrant is sodium hydroxymethyl starch, and the disintegrant can disintegrate the ingredients in the coating 100 after contacting water, thereby facilitating the dissolution of the pharmaceutical ingredients in water.
A method for the sustained release of a polyphenol drug comprising:
A. swallowing the polyphenol with water;
B. the powdered sugar particles 300 filled in the pores 200 after being swallowed are dissolved in water, and the water enters the coating 100 through the pores 200, so that the drug in the coating 100 is dissolved into a saturated solution, and the saturated solution continuously flows out from the pores 200 until the dissolution is completed due to the difference in osmotic pressure between the inside and the outside of the coating 100.
Example 2:
the scheme of example 1 is further described below in conjunction with specific working modes, which are described in detail below:
as shown in fig. 1, fig. 2 and fig. 3, the present embodiment provides a polyphenol compound drug, which comprises the following raw materials in parts by weight:
1 part of polyphenol compound, 4 parts of adhesive, 40 parts of filler and 7 parts of disintegrating agent;
the coating 100 is coated with the polyphenol compounds, the adhesive, the filler and the disintegrant, a plurality of pores 200 are formed in the outer surface of the coating 100, the powder sugar granules 300 are filled in each pore 200, and the finished product has sweet taste which has higher attraction to patients by forming the pores 200 in the outer surface of the coating 100 and filling the powder sugar granules 300 in the pores, so that the resistance of the patients to the medicaments is reduced, and the use and treatment are facilitated.
In a preferred embodiment, in addition to the above-described embodiment, the coating 100 is coated with a mixture of the polyphenol compound, the binder, the filler and the disintegrant, and the coating 100 protects the polyphenol compound, the binder, the filler and the disintegrant.
In a preferred embodiment, in addition to the above-described embodiments, the coating 100 is a polymer film, which is cellulose acetate and is insoluble in water, and after administration, enters the intestinal tract by gastrointestinal motility and is finally discharged to the outside of the body.
In a preferred embodiment, in addition to the above embodiment, the powdered sugar particles 300 are stevioside.
In a preferred embodiment, in addition to the above-mentioned embodiments, the polyphenol compound is stilbene, and the polyphenol compounds used in the present invention are all the prior art, and thus are not described again.
In a preferred embodiment, in addition to the above-mentioned embodiment, the adhesive is hypromellose, and the adhesive is used for bonding a plurality of substances together.
In a preferred embodiment, in addition to the above-described embodiment, the filler is microcrystalline cellulose, and the filler can increase the bulk volume.
In a preferred embodiment, in addition to the above embodiment, the inorganic calcium salt is calcium hydrogen phosphate.
In addition to the above embodiment, a disintegrant is low-substituted hydroxypropylcellulose, and the disintegrant can disintegrate the ingredients in the coating 100 after contacting water, thereby facilitating the dissolution of the pharmaceutical ingredients in water.
A method for the sustained release of a polyphenol drug comprising:
A. swallowing the polyphenol with water;
B. the powdered sugar particles 300 filled in the pores 200 after being swallowed are dissolved in water, and the water enters the coating 100 through the pores 200, so that the drug in the coating 100 is dissolved into a saturated solution, and the saturated solution continuously flows out from the pores 200 until the dissolution is completed due to the difference in osmotic pressure between the inside and the outside of the coating 100.
Example 3:
the schemes of examples 1 and 2 are further described below in conjunction with specific working examples, which are described in detail below:
as shown in fig. 1, fig. 2 and fig. 3, the present embodiment proposes a polyphenol compound drug, which comprises the following raw materials in parts by weight:
1.1 parts of polyphenol compound, 5 parts of adhesive, 50 parts of filler and 7 parts of disintegrating agent;
the coating 100 is coated with the polyphenol compounds, the adhesive, the filler and the disintegrant, a plurality of pores 200 are formed in the outer surface of the coating 100, the powder sugar granules 300 are filled in each pore 200, and the finished product has sweet taste which has higher attraction to patients by forming the pores 200 in the outer surface of the coating 100 and filling the powder sugar granules 300 in the pores, so that the resistance of the patients to the medicaments is reduced, and the use and treatment are facilitated.
In a preferred embodiment, in addition to the above-described embodiment, the coating 100 is coated with a mixture of the polyphenol compound, the binder, the filler and the disintegrant, and the coating 100 protects the polyphenol compound, the binder, the filler and the disintegrant.
In a preferred embodiment, in addition to the above-described embodiments, the coating 100 is a polymer film, and the polymer film, cellulose acetate, is insoluble in water, and enters the intestinal tract by gastrointestinal motility after administration, and is finally discharged from the body.
In addition to the above embodiment, the powdery sugar particles 300 are preferably aspartame, and are suitable for various people.
In a preferred embodiment, in addition to the above-mentioned embodiments, the polyphenol compound is phenolic acid, and the polyphenol compounds used in the present invention are all known in the art, and thus are not described in detail.
In a preferred embodiment, in addition to the above-described embodiment, the binder is sodium carboxymethylcellulose, and the binder is used to bind a plurality of substances together.
In a preferred embodiment, in addition to the above-described embodiment, the filler is an inorganic calcium salt, and the filler can increase the bulk volume.
In a preferred embodiment, in addition to the above embodiment, the inorganic calcium salt is calcium carbonate.
In a preferred embodiment, in addition to the above-described embodiment, the disintegrant is croscarmellose sodium, and the disintegrant enables the components in the coating 100 to disintegrate after contact with water, thereby facilitating the dissolution of the pharmaceutical ingredients in water.
A method for the sustained release of a polyphenol drug comprising:
A. swallowing the polyphenol with water;
B. the powdered sugar particles 300 filled in the pores 200 after being swallowed are dissolved in water, and the water enters the coating 100 through the pores 200, so that the drug in the coating 100 is dissolved into a saturated solution, and the saturated solution continuously flows out from the pores 200 until the dissolution is completed due to the difference in osmotic pressure between the inside and the outside of the coating 100.
Example 4:
the schemes in example 1, example 2 and example 3 are further described below in conjunction with specific working modes, which are described in detail below:
as shown in fig. 1, fig. 2 and fig. 3, the present embodiment proposes a polyphenol compound drug, which comprises the following raw materials in parts by weight:
1.2 parts of polyphenol compound, 6 parts of adhesive, 60 parts of filler and 10 parts of disintegrating agent;
the novel sugar-free tablet further comprises a coating 100, wherein the polyphenol compound, the adhesive, the filler and the disintegrating agent are wrapped in the coating 100, a plurality of fine holes 200 are formed in the outer surface of the coating 100, the powder sugar particles 300 are filled in each fine hole 200, the fine holes 200 are formed in the outer surface of the coating 100, and the powder sugar particles 300 are filled in the fine holes, so that a finished product has sweet taste, and the sweet taste has high attraction to patients, so that the rejection of the patients to medicines is reduced, and the novel sugar-free tablet is beneficial to use and treatment.
In a preferred embodiment, in addition to the above-described embodiment, the coating 100 is coated with a mixture of the polyphenol compound, the binder, the filler and the disintegrant, and the coating 100 protects the polyphenol compound, the binder, the filler and the disintegrant.
In a preferred embodiment, in addition to the above embodiment, the coating 100 is a polymer film, the polymer film is ethyl cellulose, and the polymer film is insoluble in water, and after administration, the coating enters the intestinal tract under the gastrointestinal motility and is finally discharged to the outside of the body.
In a preferred embodiment, in addition to the above-described embodiment, the powdery sugar particles 300 are erythritol, and erythritol particles are easily soluble in water, and erythritol does not participate in human sugar metabolism and is not converted into glucose in the human body, and therefore, the powdery sugar particles are suitable for various people without increasing the blood sugar level.
In a preferred embodiment, in addition to the above-mentioned embodiment, the polyphenol compound is lignan, and the polyphenol compounds used in the present invention are all known in the art, and thus are not described again.
In a preferred embodiment, in addition to the above, the binder is povidone, and the binder is used to bond a plurality of substances together.
In a preferred embodiment, in addition to the above embodiment, the filler is starch, and the filler can increase the bulk increase in weight.
In a preferred embodiment, in addition to the above embodiment, the inorganic calcium salt is calcium hydrogen phosphate.
In a preferred embodiment, in addition to the above-mentioned embodiments, the disintegrant is sodium hydroxymethyl starch, and the disintegrant can disintegrate the components in the coating 100 after contacting water, thereby facilitating the dissolution of the pharmaceutical ingredients in water.
A method for the sustained release of a polyphenol drug comprising:
A. swallowing the polyphenol with water;
B. the powdered sugar particles 300 filled in the pores 200 after being swallowed are dissolved in water, and the water enters the coating 100 through the pores 200, so that the drug in the coating 100 is dissolved into a saturated solution, and the saturated solution continuously flows out from the pores 200 until the dissolution is completed due to the difference in osmotic pressure between the inside and the outside of the coating 100.
The drugs prepared in examples 1 to 4 were tested as follows:
the test animals are: 50 KM mice, male, weighing 20g.
The test method comprises the following steps: randomly grouping the mice into groups, culturing 10 mice in each group under the same test environment for 30 days, and detecting cerebrospinal fluid beta amyloid protein and total Tau protein or phosphorylated Tau protein of the mice in each group before culturing;
the test method comprises the following steps: the drugs are placed in a tray, the number of mice which take the drugs actively is recorded, the mice which do not take the drugs actively are fed with the drugs artificially, cerebrospinal fluid beta amyloid protein and total Tau protein or phosphorylated Tau protein of each group of mice are detected again after 30 days, and the detection results are compared, wherein the results are shown in fig. 4.
The above embodiments are merely illustrative of the present invention and are not to be construed as limiting the invention. Although the present invention has been described in detail with reference to the embodiments, it should be understood by those skilled in the art that various combinations, modifications or equivalents may be made to the technical solution of the present invention without departing from the spirit and scope of the technical solution of the present invention, and the technical solution of the present invention is covered by the claims of the present invention.
Claims (10)
1. The polyphenol compound medicine is characterized by comprising the following raw materials in parts by weight:
0.5-1.2 parts of polyphenol compound, 3-6 parts of adhesive, 30-60 parts of filler and 5-10 parts of disintegrating agent;
the sugar-free tablet further comprises a coating (100), wherein the polyphenol compound, the adhesive, the filler and the disintegrant are wrapped in the coating (100), a plurality of fine holes (200) are formed in the outer surface of the coating (100), and powder sugar particles (300) are filled in each fine hole (200).
2. The polyphenolic drug of claim 1, wherein the polyphenolic compound, the binder, the filler and the disintegrant are mixed and encapsulated in a coating (100).
3. The polyphenol compound drug as claimed in claim 2, wherein the coating (100) is a polymer film, and the polymer film is ethyl cellulose or cellulose acetate.
4. The polyphenolic compound drug of claim 3, wherein the powdered sugar particles (300) are one of erythritol, steviol glycosides or aspartame.
5. The polyphenolic agent of claim 4, wherein said polyphenolic agent is one of a flavonoid, a stilbene, a phenolic acid, or a lignan.
6. The polyphenol compound drug of claim 5, wherein the binder is one of povidone, hypromellose, or sodium carboxymethylcellulose.
7. The polyphenol compound drug of claim 6, wherein the filler is one of starch, microcrystalline cellulose, or an inorganic calcium salt.
8. The polyphenol compound medicament of claim 7, wherein the inorganic calcium salt is one of calcium sulfate, calcium hydrogen phosphate or calcium carbonate.
9. The polyphenol compound medicament as claimed in claim 8, wherein the disintegrant is one of sodium hydroxymethyl starch, low-substituted hydroxypropyl cellulose or croscarmellose sodium.
10. A method for sustained release of a polyphenol compound drug using the polyphenol compound drug of claim 9, comprising:
A. swallowing the polyphenol with water;
B. after being swallowed, the powder sugar particles (300) filled in the pores (200) are dissolved in water, the water enters the coating (100) through the pores (200), so that the medicine in the coating (100) is dissolved into a saturated solution, the saturated solution continuously flows out from the pores (200) until the dissolution is finished due to the difference of the osmotic pressure inside and outside the coating (100).
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| CN202211268046.2A CN115607539A (en) | 2022-10-17 | 2022-10-17 | Polyphenol compound medicine and slow release method |
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| CN202211268046.2A CN115607539A (en) | 2022-10-17 | 2022-10-17 | Polyphenol compound medicine and slow release method |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1872160A (en) * | 2005-05-31 | 2006-12-06 | 谢洛佳 | Sloly released tablet of red sage root, and preparation method |
| CN101502518A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Glipizide sustained-release granular formulation and preparation method thereof |
| CN102579534A (en) * | 2011-04-28 | 2012-07-18 | 哈尔滨兰格药业股份有限公司 | Bear bile cardio-reliever pill sustained release preparations |
| KR20170061219A (en) * | 2015-11-25 | 2017-06-05 | 한국유나이티드제약 주식회사 | Controlled Released Hard Capsule Preparation |
-
2022
- 2022-10-17 CN CN202211268046.2A patent/CN115607539A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1872160A (en) * | 2005-05-31 | 2006-12-06 | 谢洛佳 | Sloly released tablet of red sage root, and preparation method |
| CN101502518A (en) * | 2008-09-04 | 2009-08-12 | 山东淄博新达制药有限公司 | Glipizide sustained-release granular formulation and preparation method thereof |
| CN102579534A (en) * | 2011-04-28 | 2012-07-18 | 哈尔滨兰格药业股份有限公司 | Bear bile cardio-reliever pill sustained release preparations |
| KR20170061219A (en) * | 2015-11-25 | 2017-06-05 | 한국유나이티드제약 주식회사 | Controlled Released Hard Capsule Preparation |
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